Go 6983 is a protein kinase C (PKC) inhibitor with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCζ respectively. Go 6983 inhibited intracellular Ca(2+) accumulation, suggesting a mechanism for its vasodilator properties. In vitro, Go 6983 significantly inhibited antigen-induced superoxide release from leukocytes of patients previously sensitized to tree pollen. Go 6983 (100 nM) significantly reduced PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts (P < 0.01), and significantly inhibited superoxide release from PMNs by 90 +/- 2% (P < 0.01). Go 6983 attenuated post-I/R cardiac contractile dysfunction, which may be related in part to decreased superoxide production in the presence of PMNs.
|Source||Immunobiology (2012). Figure 4. Go 6983|
|Cell Lines||Tca8113 cells|
|Incubation Time||24 h|
|Results||As shown in Fig. 4, after PKD2 was inhibited by Gö6983, IFN-γ could not induce the surface expression of PD-L1 on Tca8113.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
Gö 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury.
Young LH, et al. Cardiovasc Drug Rev. 2005 Fall;23(3):255-72. PMID: 16252018.
Protein kinase C-independent effects of protein kinase D3 in glucose transport in L6 myotubes.
Chen J, et al. Mol Pharmacol. 2005 Jan;67(1):152-62. PMID: 15496505.
Gö 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion.
Peterman EE, et al. J Cardiovasc Pharmacol. 2004 May;43(5):645-56. PMID: 15071351.
|Related PKC Products|
Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
|Zoledronic acid monohydrate
Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
Ingenol Mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
|Phorbol 12-myristate 13-acetate
Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
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